Darapladib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
斑块破裂导致包括缺血死亡、心肌梗死、急性冠脉综合征及缺血性中风的临床事件。在冠状动脉和颈动脉中，脂蛋白相关的磷脂酶A2（Lp-PLA2）似乎在这些高风险病变的发展中起主要作用。Darapladib是一种选择性的Lp-PLA 2抑制剂。
体外：Darapladib强效抑制Lp-PLA2，IC50为270 pM。已经证实，Darapladib对其他假定在动脉粥样硬化中发挥作用的分泌PLA2s没有选择性。评价1 μM的darapladib作用于人分泌PLA2s III、V和X时，达到的抑制百分比分别为0、 0和8.7％[1]。
体内：darapladib对LP-PLA2的抑制导致体内炎症的衰减，并减少载脂蛋白E缺陷小鼠斑块的形成，证明其在动脉粥样硬化发展期间的抗动脉硬化作用[2]。
临床试验：接受强化阿托伐他汀治疗的患者中，Darapladib产生持续的血浆Lp-PLA2活性抑制。IL-6及hs-CRP在160 mg的darapladib治疗12周后发生变化，表明可减少炎性负担[3]。
参考文献：
[1] Bui QT, Wilensky RL. Darapladib. Expert Opin Investig Drugs. 2010;19(1):161-8.
[2] Wang WY, Zhang J, Wu WY, Li J, Ma YL, Chen WH, Yan H, Wang K, Xu WW, Shen JH, Wang YP. Inhibition of lipoprotein-associated phospholipase A2 ameliorates inflammation and decreases atherosclerotic plaque formation in ApoE-deficient mice. PLoS One. 2011;6(8):e23425.
[3] Mohler ER 3rd, Ballantyne CM, Davidson MH, Hanefeld M, Ruilope LM, Johnson JL, Zalewski A; Darapladib Investigators. The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. J Am Coll Cardiol. 2008;51(17):1632-41.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 666.77 |
| Cas No. | 356057-34-6 |
| Formula | C36H38F4N4O2S |
| Synonyms | SB-480848;SB480848;SB 480848 |
| Solubility | ≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH |
| Chemical Name | N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide |
| SDF | Download SDF |
| Canonical SMILES | CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Darapladib (SB-480848) 是一种可逆的脂蛋白相关磷脂酶A2 (Lp-PLA2)抑制剂，IC50值为0.25 nM。 | |||||
| 靶点 | Lp-PLA2 | |||||
| IC50 | 0.25 nM | |||||
质量控制和MSDS
- 批次:
化学结构
